Overexpression of the enhancer of zeste homolog 2 (EZH2) has been found in multiple cancer types, such as myeloma, lymphoma, prostate, breast, lung or kidney cancer.
Dong Wha Pharmaceutical Co. Ltd. has defined histone-lysine N-methyltransferase EZH1 and/or EZH2 inhibitors reported to be useful for the treatment of cancer.
Previous research has demonstrated that overexpression or gain-of-function mutations of enhancer of zeste homolog 2 (EZH2) are significantly associated with tumor cell proliferation of a number of cancers.
About six months after Epizyme Inc. won FDA clearance of Tazverik (tazemetostat) for epithelial sarcoma (ES), the firm scored accelerated approval in the larger indication of relapsed or refractory (r/r) follicular lymphoma (FL). Specifically, U.S. regulators cleared the methyltransferase inhibitor for adults whose tumors test positive for an EZH2 mutation who have received at least two prior systemic therapies and for those with no satisfactory alternative treatment options – language that “gives physicians a lot of flexibility to use their clinical judgement in how to best prescribe” the drug, CEO Robert Bazemore noted.